Dermazole

Dermazole is a local and systemic antifungal drug. It is a derivative of the substances triazole and imidazole.

Indications Dermazole

The tablets are used in the systemic treatment of infectious pathologies of fungal origin, having different localizations, and caused by microbes that are sensitive to the effect of the substance ketoconazole. Among them:

• Candidal infections of the mucous membranes in the gastrointestinal tract;
• prevention of relapses or their treatment in people with chronic stage of thrush;
• therapy for systemic mycoses (including systemic candidiasis, histoplasmosis with paracoccidioidomycosis and blastomycosis);
• elimination of fungal diseases in the area of the skin and hair with nails (including candidal onychia, trichophytosis, nail mycosis, versicolor lichen, and in addition folliculitis, which has a fungal genesis), in situations where local treatment has not yielded results;
• The tablets are also used to prevent the occurrence of fungal pathologies in people with immunodeficiency.

Use of the cream - for local treatment of epidermophytosis in the limbs, as well as the groin, and at the same time for trichophytosis. In addition, the cream can be used to eliminate the following diseases:

• versicolor lichen;
• candidiasis in the skin area;
• seborrhea;
• folliculitis caused by the bacterium Pityrosporum.

Dermazole shampoo is prescribed in the following cases:

• pityriasis versicolor or pityriasis versicolor in the scalp area;
• seborrheic dermatitis or seborrheic eczema on the scalp.

Release form

Available in the form of cream, tablets and shampoo.

Cream – in tubes of 15 or 30 g. Inside a separate pack there is 1 tube of medicine.

The tablets are produced in 10 pieces inside a blister plate. In a separate package - 1-2 blisters with tablets.

The shampoo can be produced in bottles of 50 or 100 ml (1 bottle inside a pack), or in the form of sachets (volume 8 ml), 20 pieces inside a package.

Pharmacodynamics

The component ketoconazole is an artificial derivative of the substance imidazoledioxolane. It has antimycotic properties, acting against yeasts with dermatophytes.

Ketoconazole has fungistatic and fungicidal properties against eumycetes with dermatophytes, as well as yeast or dimorphic fungi. In addition, the substance has antimicrobial activity against most strains of staphylococci with streptococci.

Having penetrated the fungal cell, the medicine begins to suppress the synthesis of components that are the basis of the fungal cell membrane. In this way, the processes of biosynthesis of phospholipids with triglycerides, as well as ergosterol, are disrupted. Due to the reduction in the number of these elements inside the fungal cell, as well as the membrane itself, the structure of the cell membrane changes irreversibly. The fungistatic effect of the substance reduces the ability of the fungus to form colonies. Due to its fungicidal properties, the medicine helps to change the structure of the fungal cell membrane, as well as weaken its strength. As a result, the membrane is perforated, as a result of which the fungus dies.

Dermazole is effective in eliminating fungi caused by bacteria such as Pityrosporum orbiculare, Candida fungi, cryptococci, epidermophyton flocculosa, Trichophyton spp., and Microsporum spp., as well as infections caused by gram-positive cocci (including streptococci and staphylococci).

The substance ketoconazole has a strong fungicidal effect on the bacterium Pityrosporum ovate (it is the cause of dandruff).

After prolonged systemic use, the active component of the drug provokes a decrease in the biosynthesis of testosterone, as well as other androgenic hormones.

Pharmacokinetics

After oral administration of the tablet, the drug is well absorbed in the intestine. The efficiency of absorption increases in the presence of an acidic environment. After oral administration, ketoconazole demonstrates high bioavailability (approximately 75%).

The drug is found in high concentrations in plasma, tissues and other biological fluids. The highest levels are found in the kidneys and liver, as well as the heart muscle and lungs. The substance is able to pass through the BBB, but its levels in brain tissue are higher than those in the cerebrospinal fluid. The effectiveness of the drug depends on the dosage.

The peak plasma level of the active component of the drug is observed 1-2 hours after taking the tablet. Ketoconazole has a high degree of synthesis with plasma protein (mainly albumin).

Excretion from plasma occurs in 2 phases. In the 1st phase, the half-life is 2 hours, and in the terminal phase, it is 8 hours.

The substance undergoes metabolism, resulting in the formation of inactive decay products. The drug is excreted mainly with bile, and approximately 15% is excreted with urine. The drug is excreted both in unchanged form and in the form of inactive decay products.

Dosing and administration

Pills.

Dermazole tablets are taken orally, with food, washed down with water.

For children weighing more than 30 kg, as well as adults during the treatment of systemic fungal infections, the dosage is 200 mg (1 tablet) once a day. In case of severe course of the disease or if after some time of using the drug the patient does not show any improvement, it is allowed to increase the dose to 400 mg (2 tablets) – taken once a day.

The duration of the therapeutic course is prescribed by the attending physician, taking into account the nature of the pathology, as well as the characteristics of the patient's condition and body. You should take the tablets for at least another week after all signs of the disease have disappeared, as well as after receiving a negative result of the mycological test.

To eliminate dermatological infections of the fungal type caused by dermatophytes, the medicine should be taken for a period of 2-6 weeks.

When treating pityriasis versicolor, the course duration is usually 10 days.

For infections of the oral mucosa and skin (candidal type), the course usually lasts within 2-3 weeks.

During treatment of scalp lesions (fungal etiology), the use of the drug should continue for at least 3 weeks/maximum 2 months.

In case of nail mycosis, the course often lasts for 0.5-1 year (a more precise figure depends on the speed at which the nails grow). The course can be stopped only after the affected area of the nail has completely grown out.

During systemic mycoses, the course usually lasts from 1 to 6 months.

For treatment or prevention of relapses during chronic thrush, take 2 tablets once a day for 5 days.

To prevent the occurrence of fungal infections in people with immunodeficiency - children weighing more than 30 kg and adults need to take 2 tablets of LS once a day. Children weighing less than 30 kg should take the drug at a rate of 4-8 mg / kg per day.

It is recommended to take the tablets at the same time of day to maintain a stable level of drug concentration in the plasma. If you miss a tablet, you should take it as soon as possible, but if there are less than 4 hours left before the next dose, you should not take the missed tablet.

Cream.

The cream should be applied to the affected areas 1-2 times per day.

The duration of therapy depends on the course of the pathology, but if no improvements are noted within 4 weeks from the start of drug use, it is necessary to clarify the correctness of the diagnosis.

When treating pityriasis versicolor or candidal-type dermatological infections, the course often lasts 2-3 weeks.

When eliminating skin fungi, treatment usually lasts for a period of 3-4 weeks.

During the elimination of seborrheic dermatitis, the drug is usually used for a period of 2-4 weeks.

Before and after the procedure, you must wash your hands thoroughly.

Shampoo.

The medicine in the form of shampoo must be applied to washed damp hair, then lathered and held for several minutes, and then completely rinsed off.

For pityriasis versicolor, shampoo should be applied to the hair once a day for a period of 5 days.

For seborrheic dermatitis, the medicine is also used once a day, but over a period of 3 days.

To prevent or treat dandruff, Dermazole should be used once at intervals of 7-14 days.

Use Dermazole during pregnancy

Pregnant or lactating women can use the medicine in the form of shampoo or cream without restrictions, because ketoconazole in these dosage forms is not absorbed into the bloodstream and does not have a general effect.

But Dermazole in tablet form is completely prohibited during this period. If it is necessary to take the drug during lactation, it is necessary to stop breastfeeding for the duration of treatment - because ketoconazole penetrates into breast milk.

Contraindications

A contraindication for each form of the drug is intolerance to ketoconazole.

The tablets should not be taken by people suffering from liver pathologies.

It is also prohibited to prescribe Dermazole to a patient with porphyria.

Caution is required when used in people with adrenal insufficiency.

There is no information on the use of the drug in children.

Side effects Dermazole

As a result of systemic use of the drug, the development of the following adverse reactions was observed:

• reactions from the gastrointestinal tract and hepatobiliary system: vomiting, bowel disorders, epigastric pain and nausea. Hepatitis may also develop and the activity of liver enzymes may increase;
• manifestations from the central nervous system: dizziness and headaches, as well as photophobia;
• disturbances in the functioning of the cardiovascular system and the hematopoietic system: increased intracranial pressure, as well as the development of thrombocytopenia;
• manifestations of allergies: rashes and itching, as well as urticaria. The appearance of allergic rhinitis is observed sporadically;
• Others: development of impotence, gynecomastia or alopecia, as well as menstrual cycle disorders and the occurrence of paresthesia.

As a result of local use of the cream, itching and burning with irritation in the treatment area were observed. In case of using shampoo, hair color may change or hair loss may occur.

If the patient experiences any negative reactions, the medication should be discontinued and a doctor should be consulted.

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Overdose

Intoxication with local use.

If the cream is applied in excessive quantities, swelling or erythema may appear on the skin, and a feeling of a skin burn may also occur. These symptoms quickly disappear after discontinuing the drug.

When taking tablets, an overdose manifests itself in the form of vomiting with nausea, as well as dizziness with headache. With a further increase in dosage, a feeling of tingling and spasms may occur.

The medicine has no antidote. To eliminate the disorders, it is necessary to cancel the medicine, wash the stomach and give the victim enterosorbents. Symptomatic treatment is also used.

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Interactions with other drugs

Interaction of tablets.

Medicines that help lower the pH level in the stomach reduce the degree of absorption of ketoconazole. Therefore, in case of combined use of these drugs, it is necessary to observe intervals between doses - at least 2 hours.

Rifampicin with isoniazid in combination with Dermazole reduces the latter's levels in plasma.

Due to the blockade of liver enzymes in the hemoprotein P450 system that occurs under the influence of ketoconazole, the period of medicinal effect of drugs that are directly metabolized by these enzymes increases. Since the metabolic processes are inhibited, the likelihood of negative effects of these drugs increases.

Potentially dangerous combinations include: statins, astemizole, terfenadine with midazolam, and also cisapride with triazolam for internal use. Ketoconazole increases the levels of these drugs in plasma, which can cause negative reactions from the cardiovascular system. Therefore, taking these drugs together is prohibited.

Ketoconazole prolongs the period of sedation produced by intravenous midazolam.

When combined with Dermazole, it is necessary to adjust the dosages of cyclosporine with bisulfan, as well as anticoagulants with methylprednisolone.

Ketoconazole cannot be combined with ethyl alcohol (the combination of these agents leads to the development of a disulfiram-like effect), as a result of which it is necessary to refrain from drinking alcohol during treatment with Dermazole.

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Storage conditions

The medicine should be kept in a dark place, inaccessible to small children. Temperature conditions – maximum 25°C.

Shelf life

Dermazole is permitted to be used for a period of 3 years from the date of manufacture of the drug.